Product Details
| Product Name:
GSK1379725A |
CAS No.:
1802251-00-8 |
| Purity:
99.59% |
Supply Ability:
10g |
| Release date:
2024/11/11 |
Product Introduction
Bioactivity
| 名稱 | GSK1379725A |
| 描述 | GSK1379725A is a selective BPTF ligand [Kd = 2.8 μM]. |
| 體外活性 | GSK1379725A has proven to be selective towards Brd4, though comprehensive evaluation against other bromodomains is necessary. Searches in the ChEMBL database reveal its activity in only five cellular assays, indicating a potency (EC50) of 500 nM, with no kinase activity noted despite extensive screenings, especially with the PKIS library[1]. NMR titration data showed a separation of 171 Hz between bound and unbound resonances of GSK1379725A, suggesting a maximum chemical exchange rate. Based on an assumed high association rate (e.g., similar to chymotrypsin: proflavin at 1.2×108 M-1 s-1), the dissociation constant (Kd) is approximately 8 μM. For more precise Kd measurement, ITC was employed with unlabeled BPTF, yielding a Kd of 2.8 μM, aligning with the observed intermediate exchange resonance broadening detected by PrOF NMR, thus confirming the specificity and binding characteristics of GSK1379725A. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 50 mg/mL (111 mM), Sonication is recommended.
|
| 關鍵字 | inhibit | Inhibitor | GSK1379725A | Epigenetic Reader Domain | GSK-1379725A |
| 相關產(chǎn)品 | ABBV-744 | CeMMEC1 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | J-147 | Anacardic Acid | CTB | Curcumin | dBET6 | Piflufolastat | Naphthol AS-E | Bisdemethoxycurcumin |
| 相關庫 | 組蛋白修飾化合物庫 | 經(jīng)典已知活性庫 | 表觀遺傳庫 | 已知活性化合物庫 | 共價抑制劑庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States